Palatinose for enhancing dietary supplement and pharmaceutical delivery

ABSTRACT

The present invention is directed to a dietary supplement comprising palatinose or a derivative thereof. The dietary supplement may be a nutritional product, a sports performance product, a weight loss product or a meal replacement product. The present invention is also directed to a method of increasing the absorption of a compound into the bloodstream, cells and tissue comprising administering palatinose, or a derivative thereof, in combination with the compound. The present invention also relates to a diluent for parenteral compounds. The diluent comprises palatinose or a derivative thereof. Another aspect of the present invention is directed to a method of decreasing the recovery time to pre-performance levels of total adenosine triphosphate (ATP) levels in a mammal comprising administering palatinose, or a derivative thereof, to the mammal. The present invention is further directed to a method of supplying a compound to a diabetic patient, burn victim patient or trauma victim patient. The method comprises administering palatinose, or a derivative thereof, in combination with the compound.

BACKGROUND OF THE INVENTION 1 . Technical Field

The present invention relates to a disaccharide for therapeutic use.More particularly, the invention relates to the use of palatinose(6-O-alpha-D-glucopyranosyl-D-fructofuranose) to increase the efficacyof dietary supplements and pharmaceuticals.

2. Description of Related Art

Palatinose is 2 disaccharide consisting of d-glucose and d-fructoseconnected by an alpha-1,6-glycosidic linkage. It is also referred to as6-O-alpha-D-glucopyronosyl-D-fructofuranose and as isomaltulose, and isreadily produced commercially from sucrose by enzymatic rearrangement.Palatinose has a taste and appearance similar to that of sucrose.Because of the rate by which it is metabolized, it presents potentialdietary and therapeutic uses.

Most sugars are rapidly absorbed after consumption. Therein, after oraladministration of a significant amount of sucrose (common table sugar),blood glucose levels rise quickly. This is followed by a quick rise ininsulin levels which brings the blood glucose level back down. Thedigestion and absorption of paletinose is unlike other sugars. It iscompletely digested and absorbed at a much slower speed, equivalent toabout ⅕ of that for sucrose. Thus, alter oral administration ofpalatinose, blood glucose and insulin levels rise more slowly and reacha lower maxima compared to sucrose. Because of this characteristic,palatinose is well suited as a sucrose replacement for diabetics andothers with prediabetic dispositions.

Another benefit of palatinose is its non-cariogenic quality, i.e., doesnot promote tooth decay. It is used as a substitute for other sugars,particularly in the candy and chewing gum industry. Moreover, it is animprovement over other sugar-substitutes because it does not causeabdominal discomfort or diarrhea, a side-effect of many sugar alcohols.

Many compounds, including nutrients and dietary supplements, depend onthe presence of a sugar for absorption from the gastrointestinal tractas well as for absorption from the plasma into various tissues/cells ofthe body. Studies have demonstrated that the performance enhancingsupplement creatine is better absorbed into human skeletal muscle whentaken with glucose. Certain amino acids are also more readily absorbedwhen administered with glucose. However, sucrose and other sugars arenot ideal for use in combination with nutrient supplements. Sucrose israpidly digested and absorbed into the blood stream. This results in arapid rise in circulating insulin levels which quickly lowerscirculating glucose levels. As a result, many compounds and nutrientsadministered in combination with sucrose may not be absorbed because ofthe short duration of the “sugar effect.”

Moreover, excessive amounts of sugar can cause an increase in body fat,decreased sensitivity to insulin and tooth decay. Sugar substitutes,which are generally sugar alcohols, are also inadequate for purposes ofaiding absorption. Although they are hydrolyzed and digested slowly,they often cause abdominal discomfort and diarrhea. Thus, an improvedsugar is needed for use in the absorption of dietary supplement productsas well as other therapeutic compounds.

SUMMARY OF THE INVENTION

The present invention solves the above-described problem by providing adietary supplement comprising palatinose or a derivative thereof, asugar, a stimulant, at least one amino acid or derivative thereof, andat least one mineral. The dietary supplement may be a nutritionalproduct, a sports performance product, a weight loss product, or a mealreplacement product. Palatinose enhances absorption of the dietarysupplement components into the bloodstream, cells and tissue.

More particularly, the dietary supplement may comprise palatinose or aderivative thereof; amylose; glucose; a methylxanthine such as caffeineor theobromine or both; arginine or a salt, ester or chelate thereof;creatine or a salt, ester or chelate thereof; disodium adenosinetriphosphate; calcium carbonate; sodium bicarbonate; andglucuronolactone. This dietary supplement formulation increases theathletic performance of a mammal during an approximately one to threehour period.

Still more particularly, the dietary supplement of the present inventionmay comprise palatinose or a derivative thereof, trehalose; amylose;amylopectin; L-carnosine; calcium carbonate; sodium bicarbonate;sulbutiamine or fursultiamine; disodium adenosine triphosphate; oroticacid, vinpocetine or rhodiola rosea; and cellulose or anotherundigestible bulk forming starch. This dietary supplement formulationincreases the athletic performance of a mammal during an approximatelythree to eight hour period.

Another aspect of the present invention is directed to a method ofincreasing the absorption of a compound into the bloodstream, cells andtissue. The method includes administering palatinose or a derivativethereof in combination with the compound.

More particularly, the compound may be a dietary supplement, a nutrient,a pharmaceutical, or a vaccine. If the compound is a dietary supplementformulation, the method may comprise adding palatinose or derivativethereof to the dietary supplement formulation prior to administration.If the compound is a pharmaceutical formulation, the method may compriseadding palatinose or a derivative thereof to the pharmaceuticalformulation.

Still, another aspect of the present invention is directed to a diluentfor parenteral compounds, wherein the diluent comprises palatinose or aderivative thereof. The parenteral compound may be a dietary supplement,a nutrient, a pharmaceutical, or a vaccine.

Yet another aspect of the present invention is directed to a method ofdecreasing recovery rime to pre-performance levels of total adenosinetriphosphate (ATP) levels In a mammal comprising administeringpalatinose, or derivative thereof, to the mammal. The palatinose orderivative thereof may be administered orally or parenterally.Preferably, the palatinose or derivative thereof is administered in adose between about 0.5 grams and about 200 grams.

The present invention is also directed to a method of supplying acompound to a diabetic patient, burn victim patient or trauma victimpatient. The method includes administering palatinose, or a derivativethereof in combination with the compound. The compound may be anutrient, dietary supplement, or pharmaceutical. The compound andpalatinose or derivative thereof, may be administered orally orparenterally. In addition, the palatinose or derivative thereof ispreferably administered in a dose between about 0.5 grams and about 200grams.

Other features and advantages of the present invention will becomeapparent upon reading the following detailed description of embodimentsof the invention, when taken in conjunction with the appended claims.

DETAILED DESCRIPTION

Studies have demonstrated that the presence of sugar directly enhancesnutrient absorption into various tissues and cells. For example, amixture of arginine and glucose is more efficiently absorbed into thevascular endothelium than arginine alone. Other studies have shown thatnutrients and ergogenic sports performance products depend on theindirect presence of sugar for absorption wherein increased levels ofinsulin enhance the absorption of nutrients into the tissues and cells.

Palatinose oilers an improvement over other sugars, including glucose,in that it is metabolized much slower by the gastrointestinal tractthereby extending the time that the “sugar effect,” both direct andindirect, can have on the absorption of dietary supplements, nutrients,pharmaceuticals or vaccines. Rather than enter the blood stream, rapidlyrise and fall, palatinose leads to gradual increases and sustainedlevels of glucose and insulin. This allows greater time and opportunityfor the absorption of various compounds. With respect to dietarysupplements, the end result may be greater energy, alertness, athleticperformance and/or muscle development.

Moreover, replacing common sugars with palatinose presents otheradvantages. Preventing surges in blood glucose and insulin levels mayhelp in the management and prevention of obesity, diabetes andcardiovascular disease. Recent studies have also provided evidence thatpalatinose may also have a positive effect on mental concentration. Andunlike other sugars, palatinose does not promote tooth decay.

The Dietary Supplement Health and Education Act of 1994, commonlyreferred to as DSHEA, defines “dietary supplement” as my product (excepttobacco) that contains at least one of the following: (1) a vitamin, (2)a mineral, (3) an herb or botanical, (4) an amino acid, (5) a dietarysubstance “for use to supplement the diet by increasing total dietaryintake,” or (6) any concentrate, metabolite, constituent, extract, orcombination of any of the aforementioned ingredients. Examples ofdietary supplements include, but are not limited to nutritionalproducts; sports performance products, including ergogenic sportsperforming products; weight loss products; and meal replacementproducts. Dietary supplements may exist in various forms, including, butnot limited to tablets, capsules, caplets, powders, drinks includingshakes, solid food items including snack bars, etc.

In one embodiment, the dietary supplement of the present inventionincludes palatinose or a derivative thereof, a sugar, a stimulant, atleast one amino acid or derivative thereof, and at least one mineral.For example, a dietary supplement designed to increase the athleticperformance of a mammal during a one to three hour sports activityperiod, preferably comprises palatinose or a derivative thereof;amylose; glucose, a methylxanthine such as caffeine or theobromine orboth; arginine or a salt, ester or chelate thereof; creatine or a salt,ester or chelate thereof; disodium adenosine triphosphate; calciumcarbonate; sodium bicarbonate; and glucuronolactone.

Alternatively, the dietary supplement of the present invent ion maycomprise palatinose or a derivative thereof; trehalose; amylose;amylopectin; L-carnosine; calcium carbonate: sodium bicarbonate,sulbutiamine or fursultiamine; disodium adenosine phosphate, oroticacid; vinpocetine or rhodiola rosea; cellulose or another undigestiblebulk forming starch; and perhaps at least one B vitamin. This dietarysupplement formulation increases the athletic performance of a mammalduring an approximately three to eight hour period.

Other preferred dietary supplement formulations of the preset inventionmay comprise palatinose or a derivative thereof, and any or all of thefollowing: water; carbon dioxide; creatine or a salt, ester or chelatethereof; carnitine or a salt, ester or chelate thereof; taurine or asalt, ester or chelate thereof; carnosine or a salt, ester or chelatethereof; citrulline or a salt, ester or chelate thereof; carnosine or asalt, ester or chelate thereof; pyruvate or a salt, ester or chelatethereof; ribose; amylase; amylopectine; tyrosine or a salt, ester orchelate thereof; tyramine or a salt, ester or chelate thereof; histidineor a salt, ester or chelate thereof; alanine or a salt, ester or chelatethereof; phenylalanine or a salt, ester or chelate thereof; adenosinemono, di or triphosphate, or a salt, ester or chelate thereof; alphalipoic acid, or a salt, ester or chelate thereof; 4-hydroxy-isoleucine,d-pinitol; ornithine or a salt, ester or chelate thereof; sodium or anysalt thereof; potassium or any salt thereof; zinc or any salt thereof;magnesium or any salt thereof; iron or any salt thereof; chromium or anysalt thereof; calcium or any salt thereof; vitamin B-1; vitamin B-2;vitamin B-3; vitamin B-6; vitamin B-12; pantothenic acid, folic acid;vitamin C; 7-keto-DHEA, or any ester or ether thereof; 7-hydroxy-DHEA orany ester thereof; caffeine; octopamine; norsynephrine; synephrine;ephedrine; hordenine; theobromine; evodiamine; phenylephrine; insulin;metformin; corosolic acid; glucuronolactone; ginger; ginseng; ginkobiloba; rhodiola roses; fenugreek; epicatechin; epicatechin-3-gallate;epigallocatechin; epigallocatecin-3-gallate; glutamine; branched chainamino acids or any salts or esters thereof, any chelate of any aminoacid; 6-methyluracil; phosphocreatinine; orotic acid;5-hydroxytrypiophan; vinpocetine, sucralose; fructose; galactose:maltodextrin; glucose; DMAE; DMG; TMG; coenzyme Q-10,sulbutiamine;fursultiamine; octotiamine; adrafanil; choline; phosphatidylcholine; andphosphatidylserine.

Due to the presence of palatinose, or derivative thereof, in the dietarysupplements of the present invention, these dietary supplements increaseathletic performance, energy, strength, percent fat-free muscle mass,muscle development, mental concentration and alertness, and stamina inmammals.

It should be understood that palatinose may be added to any dietarysupplement formulation to enhance the effects of and improve theabsorption of the dietary supplement, and the present invention isintended to encompass such improved formulations. It should also beunderstood that use of the palatinose in any of the embodiments ormethods of the present invention may be substituted by any derivative ofpalatinose.

Preferably, the concentration of palatinose or derivative thereof, inthe dietary supplement is between approximately 1% and approximately85%. More preferably, the concentration of palatinose in the dietarysupplement is between approximately 10% and approximately 50%.Furthermore, the palatinose present in the dietary supplement isdesirably administered in a dose between about 0.5 grams and about 200grams.

The present invention is also related to a method of increasing theabsorption of a compound into the bloodstream, cells and tissue byadministering palatinose, or a derivative thereof, in combination withthe compound. Palatinose may be used to increase the absorption of anycompound in the method of the present invention, including compoundsused to treat any disease or illness. Exemplary compounds for use in thepresent invention include, but are not limited to a dietary supplement,a nutrient, a pharmaceutical, or a vaccine. When palatinose is used toincrease the absorption of particular compounds, including dietarysupplements and nutrients, the fatigue associated with an athleticperformance of a mammal is reduced.

In addition, because palatinose maintains a more constant elevation ofbipod sugar levels as opposed to other sugars, an optimal maximum rateof adenosine triphosphate (ATP) synthesis in cells can be maintained forseveral hours. Most sugars, including glucose, peak in the plasma about45 to 60 minutes post absorption and then then an insulin spike drivesthis level down rapidly, leading to pre-prandial (or lower) levels ofplasma sugar. When the plasma sugar levels decrease, ATP synthesis alsodecreases. Palatinose maintains a slightly heightened plasma sugar levelfor a longer period of time. As a result mitochondria have access tooptimal levels of carbohydrates for approximately 6 to 8 hours, therebyallowing for heightened and continued ATP synthesis. Accordingly, theadministration of palatinose, or a derivative thereof, to a mammaldecreases the recovery time to pre-activity performance levels of totalATP in the mammal. Preferably, palatinose is administered prior to thesports performance.

The method of the present invention may include adding palatinose, or aderivative thereof, to a dietary supplement formulation, pharmaceuticalformulation or vaccine formulation prior to administering the respectivecompounds. Preferably, the concentration of palatinose or derivativethereof, in the dietary supplement, pharmaceutical, vaccine or otherformulation, is between approximately 1% and approximately 85%. Morepreferably, the concentration of palatinose or derivative thereof, inthe dietary supplement, pharmaceutical, vaccine or other formulation, isbetween approximately 10% and approximately 50%. Furthermore, thepalatinose, or derivative thereof, is desirably administered in a dosebetween about 0.5 grams and about 200 grams.

Additional examples of compounds that may be used in the method of thepresent invention include, but are not limited to phosphatidyserine;S-adenosly-methionine, nicotinamide adenine dinucleotide; anycephalosporin antibiotic; any macrolide antibiotic; any aminoglycoside;antibiotic; any penicillin antibiotic; any fluroquinolone antibiotic;any tetracycline antibiotic; chloramphenicol; any protease inhibitorantiviral; any nucleoside analog antiviral; any reverse transcriptaseinhibitor antiviral; any polyene or membrane active antimycotic; anyazole or inhibitor of ergosterol biosynthesis antimycoties;griseofulvin; flucytosine; capsofungin; myeafungin; any pneuraminidaseinhibitor antiviral; any polymerase inhibitor antiviral; any class ofinterferon; any class of interleukin; any type of human growth hormone;any type of insulin growth factor or insulin like growth factor; anytype of anti-vascular endothelial growth factor antibodies; anyalkylating agent including those used to treat cancer of any type; anyantimetabolite agent including those used to treat cancer of any type;any plant alkaloid agent including those used to treat cancer of anytype; doxorubicin or any salt, ester, or chelate thereof; mitoxanetroneor any salt, ester or chelate thereof; bleomycin or any salt, ester,ether or chelate thereof; platinum or any salt, ester, ether or chelatethereof: paclitaxel; docetaxel; epoeitin alfa; and darbaepoetin alfa.

The compound and palatinose may be administered by any method known tothose having skill in the art including, but not limited to oral andparenteral administration. The compound and palatinose may also beadministered in a solution of water or saline, wherein the saline ishypotonic, hypertonic or normotonic saline. Palatinose, or a derivativethereof, may also be used as a diluent for any parenteral compound,including, but not limited to dietary supplements, nutrients,pharmaceuticals and vaccines.

Palatinose is particularly useful for supplying any compound, includingnutrients and pharmaceuticals, to patients, such as diabetic, burnvictim, and trauma victim patients.

It should be understood that the foregoing relates to exemplaryembodiments of the invention and that modifications may be made withoutdeparting from the spirit and scope of the invention as set forth in thefollowing claims.

What is claimed is:
 1. A dietary supplement comprising isomaltulose andcarnitine or a salt, ester or chelate thereof, wherein the concentrationof isomaltulose is between about 10% and about 85%, and wherein thedietary supplement is in a form selected from the group consisting of atablet, capsule, powder or drink.
 2. The dietary supplement of claim 1,wherein the dietary supplement is a nutritional product, a sportsperformance product, a weight loss product, or a meal replacementproduct.
 3. The dietary supplement of claim 1, wherein the concentrationof carnitine is between about 10% and about 50%.
 4. The dietarysupplement of claim 1, further comprising one or more compounds selectedfrom the group consisting of a sugar, a stimulant, an amino acid, and amineral.
 5. The dietary supplement of claim 1, further comprising one ormore compounds selected from the group consisting of trehalose; amylose;glucose; a methylxanthine; arginine or a salt, ester or chelate thereof;amylopectin; L-carnosine; calcium carbonate; sodium bicarbonate;glucuronolactone; sulbutiamine or fursultiamine; disodium adenosinephosphate; adenosine triphosphate; orotic acid; vinpocetine or rhodiolarosea; cellulose; and starch.
 6. The dietary supplement of claim 1,further comprising one or more compounds selected from the groupconsisting of citrulline or a salt, ester or chelate thereof; taurine ora salt, ester or chelate thereof; arginine or a salt, ester or chelatethereof; carnosine or a salt, ester or chelate thereof; pyruvate or asalt, ester or chelate thereof; tyrosine or a salt, ester or chelatethereof; tyramine or a salt, ester or chelate thereof; histidine or asalt, ester or chelate thereof; alanine or a salt, ester or chelatethereof; phenylalanine or a salt, ester or chelate thereof;4-hydroxy-isoleucine; ornithine or a salt, ester or chelate thereof;glutamine; branched chain amino acids or a salt, ester or chelatethereof; an amino acid chelate; 5-hydroxy-tryptophan; and choline. 7.The dietary supplement of claim 1, further comprising Coenzyme Q-10 andone or more of creatine, a creatine salt, a creatine ester and acreatine chelate.
 8. The dietary supplement of claim 1, furthercomprising one or more of creatine, a creatine salt, a creatine esterand a creatine chelate.
 9. The dietary supplement of claim 1, furthercomprising coenzyme Q10.
 10. The dietary supplement of claim 1, furthercomprising one or more stimulants.
 11. The dietary supplement of claim10, wherein the one or more stimulants are selected from the groupconsisting of caffeine; octopamine; norsynephrine; synephrine;ephedrine; hordenine; theobromine; sulbutiamine; fursultiamine;octotiamine; and adrafanil.
 12. The dietary supplement of claim 1,further comprising carbon dioxide.
 13. A method of increasing theabsorption of carnitine or a salt, ester or chelate thereof into thebloodstream of a mammal, wherein the method comprises administering tothe mammal a composition comprising isomaltulose and carnitine or asalt, ester or chelate thereof.
 14. The method of claim 13, wherein thecomposition is selected from the group consisting of a dietarysupplement, a nutrient or a pharmaceutical.
 15. The method of claim 13,wherein the composition is in a form selected from the group consistingof a tablet, capsule, powder or drink.
 16. The method of claim 13,wherein the concentration of isomaltulose in the composition is betweenabout 10% and about 85%.
 17. The method of claim 13, wherein theconcentration of isomaltulose in the composition is between about 10%and about 50%.
 18. The method of claim 13, wherein the compositioncomprises between about 0.5 grams and about 200 grams of isomaltulose.19. The method of claim 13, wherein the composition further comprisesone or more of creatine, a creatine salt, a creatine ester and acreatine chelate.
 20. The method of claim 13, wherein the compositionfurther comprises one or more compounds selected from the groupconsisting of a sugar; a stimulant; creatine or a salt, ester or chelatethereof; coenzyme Q-10; 7-keto-DHEA; a mineral; an undigestiblebulk-forming starch; adenosine triphosphate; carbon dioxide; trehalose;amylose; glucose; a methylxanthine; amylopectin; calcium carbonate;sodium bicarbonate; glucuronolactone; sulbutiamine; fursultiamine;orotic acid; vinpocetine; rhodiola rosea; and cellulose.